US5962493AExpiredUtility
2-mercaptobenzimidazole derivatives and antihyperlipemic agent or antiarteriosclerotic agent containing the same
Est. expiryFeb 4, 2014(expired)· nominal 20-yr term from priority
A61K 31/4184A61P 3/06A61P 9/10C07D 235/28
30
PatentIndex Score
0
Cited by
21
References
10
Claims
Abstract
2-Mercaptobenzimidazole derivatives represented by the following formulae, analogs and salts thereof are disclosed: ##STR1## These 2-mercaptobenzimidazole derivatives are useful as a medicine such as an antihyperlipemic agent or antiarteriosclerotic agent and also useful as an additive for silver halide photosensitive materials, liquid crystals and the like.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1. A method for inhibiting hyperlipemia or atherosclerosis comprising administering an effective amount of a 2-mercaptobenzimidazole compound represented by formula IV: ##STR13## wherein R 3 and R 4 each represent a hydrogen atom, a halogen atom, or an alkyl, alkoxy, alkoxycarbonyl, carbamoyl, sulfamoyl, acylamino, sulfonylamino, cyano or nitro group; R 50 and R 60 each represent a hydrogen atom, alkyl group, or acyl group; n 3 , n 4 , each represent 1 or 2; and L 2 represents a connecting group which is an alkylene group or a phenylene group-containing an alkylene group, or a pharmaceutically acceptable salt thereof, to a mammal.
2. The method of claim 1, wherein the 2-mercaptobenzimidazole compound is a compound represented by formula IV-a: ##STR14## wherein L 2 , R 50 and R 60 are as defined in claim 1, R 31 and R 32 are the same as R 3 , and R 41 and R 42 are the same as R 4 .
3. The method of claim 2, wherein R 31 , R 32 , R 41 , R 42 , R 50 and R 60 in formula IV-a are hydrogen, and L 2 is an alkylene group having 4 to 10 carbon atoms or an alkylene-phenylene-alkylene group wherein each alkylene moiety of the alkylene-phenylene-alkylene group has 1 to 2 carbon atoms.
4. The method of claim 2, wherein one of R 31 and R 32 and one of R 41 and R 42 in formula IV-a are hydrogen, and the other one of R 31 and R 32 and the other one of R 41 and R 42 are lower alkyl, halogen, nitro or lower acylamino, and R 50 and R 60 are hydrogen, lower alkyl or lower alkanoyl.
5. The method of claim 2, wherein R 31 , R 32 , R 41 and R 42 in formula IV-a are halogen, and R 50 and R 60 are hydrogen.
6. The method of claim 2, wherein R 31 , R 32 , R 41 and R 42 in formula IV-a are hydrogen, and R 50 and R 60 are lower alkanoyl or lower alkyl, and L 2 is an alkylene group having 4 to 10 carbon atoms or an alkylene-phenylene-alkylene group, wherein each alkylene moiety of the alkylene-phenylene-alkylene group has 1 to 2 carbon atoms.
7. The method of claim 2, wherein R 31 , R 32 , R 41 and R 42 in formula IV-a are halogen or lower alkyl, and R 50 and R 60 are lower alkanoyl or lower alkyl.
8. A method for therapy of hyperlipemia or atherosclerosis in a mammal comprising administering an effective amount of a 2-mercaptobenzimidazole compound represented by formula IV: ##STR15## wherein R 3 and R 4 each represent a hydrogen atom, halogen atom, or alkyl, alkoxy, alkoxycarbonyl, carbamoyl, sulfamoyl, acylamino, sulfonylamino, cyano or nitro group; R 50 and R 60 each represent a hydrogen atom, alkyl group, or acyl group; n 3 , n 4 each represent 1 or 2; and, L 2 represents a connecting group which is an alkylene group or phenylene group-containing alkylene group, or a pharmaceutically acceptable salt thereof, to a mammal.
9. A method for inhibiting foamy macrophages in a mammal comprising contacting a foamy macrophage with an effective amount of a 2-mercaptobenzimidazole compound represented by formula IV: ##STR16## wherein R 3 and R 4 each represent a hydrogen atom, a halogen atom, or an alkyl, alkoxy, alkoxycarbonyl, carbamoyl, sulfamoyl, acylamino, sulfonylamino, cyano or nitro group; R 50 and R 60 each represent a hydrogen atom, alkyl group, or acyl group; n 3 , n 4 each represent 1 or 2; and L 2 represents a connecting group which is an alkylene group or a phenylene group-containing an alkylene group, or a pharmaceutically acceptable salt.
10. A method for reducing the formation of cholesteryl ester in foamy macrophages in a mammal comprising contacting a foamy macrophage with an effective amount of a 2-mercaptobenzimidazole compound represented by formula IV: ##STR17## wherein R 3 and R 4 each represent a hydrogen atom, a halogen atom, or an alkyl, alkoxy, alkoxycarbonyl, carbamoyl, sulfamoyl, acylamino, sulfonylamino, cyano or nitro group; R 50 and R 60 each represent a hydrogen atom, alkyl group, or acyl group; n 3 , n 4 each represent 1 or 2; and L 2 represents a connecting group which is an alkylene group or a phenylene group-containing an alkylene group, or a pharmaceutically acceptable salt thereof.Cited by (0)
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